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  • Title: U-37883A potently inhibits dopamine-modulated K+ channels on rat striatal neurons.
    Author: Lin YJ, Chen X, Freedman JE.
    Journal: Eur J Pharmacol; 1998 Jul 10; 352(2-3):335-41. PubMed ID: 9716371.
    Abstract:
    An 85 pS K+ channel of rat caudate-putamen neurons, which is activated by dopamine D2 receptors and inhibited by sulfonylurea drugs, was studied using cell-attached patch-clamp electrophysiology. This channel was inhibited by externally-applied U-37883A (4-morpholinecarboximidine-N-1-adamantyl-N'-cyclohexyl hydrochloride), a blocker of vascular ATP-sensitive K+ channels, with a half-maximal effect at a concentration of approximately 0.1 microM. Channel inhibition occurred in a time-dependent fashion when U-37883A was applied to the membrane from a back-filled patch pipette. Inhibition was associated with a decrease in fractional open time, but was voltage-insensitive and did not alter channel conductance, suggesting an effect on channel gating at a site largely insensitive to the electrical field of the channel. U-37883A was about 50 times more potent at inhibiting this channel than was the sulfonylurea drug glibenclamide. This relative potency, opposite to that found in pancreatic tissue, indicates that U-37883A is a useful tool to distinguish amongst different subtypes of sulfonylurea-sensitive K+ channels.
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